Development of inhibitors for uPAR: blocking the interaction of uPAR with its partners.

• uPAR is a cell surface receptor with diverse functions. • Plasma uPAR level is typically low and high level is associated with health crisis. • The pleiotropic functions of uPAR correspond to its interaction with various partners. • Specific inhibitors intervening with uPAR binding to its partners are summarized. Urokinase-type plasminogen activator receptor (uPAR) mediates a multitude of biological activities, has key roles in several clinical indications, including malignancies and inflammation, and, thus, has attracted intensive research over the past few decades. The pleiotropic functions of uPAR can be attributed to its interaction with an array of partners. Many inhibitors have been developed to intervene with the interaction of uPAR with these partners. Here, we review the development of these classes of uPAR inhibitor and their inhibitory mechanisms to promote the translation of these inhibitors to clinical applications. [ABSTRACT FROM AUTHOR]